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https://www.readbyqxmd.com/read/28822347/screening-and-confirmation-of-steroids-and-nitroimidazoles-in-urine-blood-and-food-matrices-sample-preparation-methods-and-liquid-chromatography-tandem-mass-spectrometric-separations
#1
Ádám Tölgyesi, Enikő Barta, Andrea Simon, Thomas J McDonald, Virender K Sharma
Veterinary drugs containing synthetic anabolic steroid and nitroimidazole active agents are not allowed for their applications in livestock of the European Union (EU). This paper presents analyses of twelve selected steroids and six nitroimidazole antibiotics at low levels (1.56μg/L-4.95μg/L and 0.17μg/kg-2.14μg/kg, respectively) in body fluids and egg incurred samples. Analyses involved clean-up procedures, high performance liquid chromatography (HPLC) separation, and tandem mass spectrometric screening and confirmatory methods...
August 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28820955/integration-of-an-in-situ-maldi-based-high-throughput-screening-process-a-case-study-with-receptor-tyrosine-kinase-c-met
#2
Katrin Beeman, Jens Baumgärtner, Manuel Laubenheimer, Karlheinz Hergesell, Martin Hoffmann, Ulrich Pehl, Frank Fischer, Jan-Carsten Pieck
Mass spectrometry (MS) is known for its label-free detection of substrates and products from a variety of enzyme reactions. Recent hardware improvements have increased interest in the use of matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) MS for high-throughput drug discovery. Despite interest in this technology, several challenges remain and must be overcome before MALDI-MS can be integrated as an automated "in-line reader" for high-throughput drug discovery. Two such hurdles include in situ sample processing and deposition, as well as integration of MALDI-MS for enzymatic screening assays that usually contain high levels of MS-incompatible components...
August 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28820893/a-computational-method-for-the-identification-of-candidate-drugs-for-non-small-cell-lung-cancer
#3
Lei Chen, Jing Lu, Tao Huang, Yu-Dong Cai
Lung cancer causes a large number of deaths per year. Until now, a cure for this disease has not been found or developed. Finding an effective drug through traditional experimental methods invariably costs millions of dollars and takes several years. It is imperative that computational methods be developed to integrate several types of existing information to identify candidate drugs for further study, which could reduce the cost and time of development. In this study, we tried to advance this effort by proposing a computational method to identify candidate drugs for non-small cell lung cancer (NSCLC), a major type of lung cancer...
2017: PloS One
https://www.readbyqxmd.com/read/28820706/high-prevalence-of-treponema-pallidum-infection-in-brazilian-prisoners
#4
Maisa Estopa Correa, Julio Croda, Ana Rita Coimbra Motta de Castro, Sandra Maria do Valle Leone de Oliveira, Maurício Antonio Pompilio, Ronaldo Omizolo de Souza, Júlio Henrique Ferreira de Sá Queiroz, Kesia Esther da Silva, Albert L Ko, Simone Simionatto
The number of new syphilis cases in Brazil has risen alarmingly in recent years. However, there is limited data regarding syphilis prevalence in the Brazilian prison population. To facilitate the development of effective interventions, a cross-sectional study was undertaken to determine the prevalence of Treponema pallidum infection, active syphilis, and associated risk factors among Brazilian prisoners. We administered a questionnaire to a population-based sample of prisoners from 12 prisons in Central-West Brazil and collected sera for syphilis testing, from January to December 2013...
July 31, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28819231/in-vitro-micropatterned-human-pluripotent-stem-cell-test-%C3%A2%C2%B5p-hpst-for-morphometric-based-teratogen-screening
#5
Jiangwa Xing, Yue Cao, Yang Yu, Huan Li, Ziwei Song, Hanry Yu
Exposure to teratogenic chemicals during pregnancy may cause severe birth defects. Due to high inter-species variation of drug responses as well as financial and ethical burdens, despite the widely use of in vivo animal tests, it's crucial to develop highly predictive human pluripotent stem cell (hPSC)-based in vitro assays to identify potential teratogens. Previously we have shown that the morphological disruption of mesoendoderm patterns formed by geometrically-confined cell differentiation and migration using hPSCs could potentially serve as a sensitive morphological marker in teratogen detection...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28819179/identification-of-polo-like-kinases-as-potential-novel-drug-targets-for-influenza-a-virus
#6
Marie O Pohl, Jessica von Recum-Knepper, Ariel Rodriguez-Frandsen, Caroline Lanz, Emilio Yángüez, Stephen Soonthornvacharin, Thorsten Wolff, Sumit K Chanda, Silke Stertz
In recent years genome-wide RNAi screens have revealed hundreds of cellular factors required for influenza virus infections in human cells. The long-term goal is to establish some of them as drug targets for the development of the next generation of antivirals against influenza. We found that several members of the polo-like kinases (PLK), a family of serine/threonine kinases with well-known roles in cell cycle regulation, were identified as hits in four different RNAi screens and we therefore studied their potential as drug target for influenza...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28818799/an-ultrafiltration-and-high-performance-liquid-chromatography-coupled-with-diode-array-detector-and-mass-spectrometry-approach-for-screening-and-characterizing-thrombin-inhibitors-from-rhizoma-chuanxiong
#7
Qian Zhang, Yu-Xiu Yang, Su-Ying Li, Ya-Li Wang, Feng-Qing Yang, Hua Chen, Zhi-Ning Xia
Thrombin (THR) plays a significant role in thromboembolic diseases, direct THR inhibitors are a class of important clinical anticoagulant drugs. This study established a THR in-solution based biospecific extraction combined with ultrafiltration and high performance liquid chromatography coupled with diode array detector and mass spectrometry analysis (TUA) method to screen and identify ligands for THR in Rhizoma Chuanxiong. After evaluating the reliability of the present TUA method using positive (argatroban) and negative (adenosine, tirofiban, ticagrelor) control drugs, this method was successfully applied to detect eight potential active compounds in Rhizoma Chuanxiong...
August 4, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28817974/applications-of-the-real-time-quaking-induced-conversion-assay-in-diagnosis-prion-strain-typing-drug-pre-screening-and-other-amyloidopathies
#8
Niccolò Candelise, Matthias Schmitz, Susana Margarida da Silva Correia, Aman Arora, Anna Villar-Piqué, Saima Zafar, Franc Llorens, Maria Cramm, Inga Zerr
The development of in vitro protein misfolding amplification assays for the detection and analysis of abnormally folded proteins, such as proteinase K resistant prion protein (PrP(res)) was a major innovation in the prion field. In prion diseases, these types of assays imitate the pathological conversion of the cellular PrP (PrP(C)) into a proteinase resistant associated conformer or amyloid, called PrP(res). Areas covered: The most prominent protein misfolding amplification assays are the protein misfolding cyclic amplification (PMCA), which is based on sonication and the real-time quaking-induced conversion (RT-QuIC) technique based on shaking...
August 18, 2017: Expert Review of Molecular Diagnostics
https://www.readbyqxmd.com/read/28816925/treatment-of-diabetic-ketoacidosis-associated-with-antipsychotic-medication-literature-review
#9
Antonia Vuk, Maja Baretic, Martina Matovinovic Osvatic, Igor Filipcic, Nikolina Jovanovic, Martina Rojnic Kuzman
BACKGROUND: The second-generation antipsychotics (SGAs) are associated with metabolic disturbances. Diabetic ketoacidosis (DKA) is a rare, but potentially fatal sign of acute glucose metabolism dysregulation, which may be associated with the use of SGAs. This study aims to review published reports of patients with schizophrenia and antipsychotic drug-associated DKA, focusing on the effective management of both conditions. METHODS: Using a predefined search strategy, we searched PubMed and EMBASE from their inception to July 2016...
August 15, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28815876/a-treatment-development-study-of-a-cognitive-and-mindfulness-based-therapy-for-adolescents-with-co-occurring-post-traumatic-stress-and-substance-use-disorder
#10
Lisa R Fortuna, Michelle V Porche, Auralyd Padilla
OBJECTIVE: Substance use is common among adolescents with post-traumatic stress disorder (PTSD). We aimed to develop and study an integrated treatment for adolescents with co-occurring disorders. DESIGN: This is a therapy development and open pilot trial study of a manualized therapy for adolescents with post-traumatic stress, depression, and substance use that uses a combination of cognitive therapy (CT) and mindfulness. METHODS: Descriptive statistics and paired sample t-tests were calculated to assess for changes in PTSD symptoms, depression, and substance use frequency from baseline to end of treatment using standardized measures and validated by urine drug screens...
August 16, 2017: Psychology and Psychotherapy
https://www.readbyqxmd.com/read/28815274/a-new-metabolomics-based-strategy-for-identification-of-endogenous-markers-of-urine-adulteration-attempts-exemplified-for-potassium-nitrite
#11
Andrea E Steuer, Kim Arnold, Tom D Schneider, Michael Poetzsch, Thomas Kraemer
Urine adulteration to circumvent positive drug testing represents a problem for toxicological laboratories. While creatinine is a suitable marker for dilution, detection of chemicals is often performed by dipstick tests associated with high rates of false positives. Several methods would be necessary to check for all possible adulterants. Untargeted mass spectrometry (MS) methods used in metabolomics should theoretically allow detecting concentration changes of any endogenous urinary metabolite or presence of new biomarkers produced by chemical adulteration...
August 16, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28814957/induced-pluripotent-stem-cell-for-the-study-and-treatment-of-sickle-cell-anemia
#12
Luiza Cunha Junqueira Reis, Virgínia Picanço-Castro, Bárbara Cristina Martins Fernandes Paes, Olívia Ambrozini Pereira, Isabela Gerdes Gyuricza, Fabiano Tófoli de Araújo, Mariana Morato-Marques, Lílian Figueiredo Moreira, Everton de Brito Oliveira Costa, Tálita Pollyanna Moreira Dos Santos, Dimas Tadeu Covas, Lygia da Veiga Pereira Carramaschi, Elisa Maria de Sousa Russo
Sickle cell anemia (SCA) is a monogenic disease of high mortality, affecting millions of people worldwide. There is no broad, effective, and safe definitive treatment for SCA, so the palliative treatments are the most used. The establishment of an in vitro model allows better understanding of how the disease occurs, besides allowing the development of more effective tests and treatments. In this context, iPSC technology is a powerful tool for basic research and disease modeling, and a promise for finding and screening more effective and safe drugs, besides the possibility of use in regenerative medicine...
2017: Stem Cells International
https://www.readbyqxmd.com/read/28814943/comparison-of-different-laboratory-tests-in-the-evaluation-of-hemorrhagic-risk-of-patients-using-rivaroxaban-in-the-critical-care-setting-diagnostic-accuracy-study
#13
Marjorie Paris Colombini, Priscilla Bento Matos Cruz Derogis, Valdir Fernandes de Aranda, João Carlos de Campos Guerra, Nelson Hamerschlak, Cristóvão Luis Pitangueiras Mangueira
BACKGROUND: Rivaroxaban is a direct oral anticoagulant designed to dispense with the necessity of laboratory monitoring. However, monitoring rivaroxaban levels is necessary in certain clinical conditions, especially in the critical care setting. METHODS: This is a diagnostic accuracy study evaluating sensitivity and specificity of prothrombin time (PT), activated partial thromboplastin time (aPTT), and Dilute Russell viper venom time (dRVVT), to evaluate the hemorrhagic risk in patients taking rivaroxaban...
2017: Thrombosis Journal
https://www.readbyqxmd.com/read/28814239/homology-modeling-and-molecular-docking-studies-of-bacillomycin-and-iturin-synthetases-with-novel-ligands-for-the-production-of-therapeutic-lipopeptides
#14
Jujjavarapu Satya Eswari, Swasti Dhagat, Shubham Kaser, Anoop Tiwari
BACKGROUND: Lipopeptide synthetases play an important role in the production of lipopeptides. Lipopeptides are molecules made up of peptides and fatty acid moieties and have shown to have a broad range of antimicrobial activity. As infectious diseases have caused severe health problems mainly resulting from the development of antibiotic resistant strains of disease causing microorganisms there is a need of alternatives to antibiotics. The lipopeptide synthetase of the corresponding lipopeptides can be used as templates to design these as drugs using computational techniques...
August 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28814125/recreational-drug-use-at-a-major-music-festival-trend-analysis-of-anonymised-pooled-urine
#15
Lotte Christine Groth Hoegberg, Cecilie Christiansen, Jesper Soe, Rasmus Telving, Mette Findal Andreasen, Dan Staerk, Lona Louring Christrup, Kenneth Thermann Kongstad
OBJECTIVE: The spread of new psychoactive substances (NPS) has expanded rapidly in the last decade. The complexity of the pharmacological effects of NPS challenges the traditional treatment guidelines, and information of the emergence of new arrivals is valuable. Our knowledge on the actual range of recreational drugs used and NPS available in Denmark is limited as identification is possible only when consumers become patients in the healthcare system or through drug seizures. We aimed to detect classical recreational drugs and NPS in the urine of music festival attendees and evaluate if the use of NPS could have been predicted by comparing study data with drug seizure data from the previous year published by European and Danish health authorities...
August 17, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28811180/development-of-an-opioid-self-administration-assay-to-study-drug-seeking-in-zebrafish
#16
Gabriel D Bossé, Randall T Peterson
The zebrafish (Danio rerio) has become an excellent tool to study mental health disorders, due to its physiological and genetic similarity to humans, ease of genetic manipulation, and feasibility of small molecule screening. Zebrafish have been shown to exhibit characteristics of addiction to drugs of abuse in non-contingent assays, including conditioned place preference, but contingent assays have been limited to a single assay for alcohol consumption. Using inexpensive electronic, mechanical, and optical components, we developed an automated opioid self-administration assay for zebrafish, enabling us to measure drug seeking and gain insight into the underlying biological pathways...
August 12, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28810948/development-and-validation-of-a-robust-and-efficient-hplc-method-for-the-simultaneous-quantification-of-levodopa-carbidopa-benserazide-and-entacapone-in-complex-matrices
#17
Erik Wollmer, Sandra Klein
PURPOSE: A variety of fixed-dose combination products is used in the therapy of Parkinson Disease. However, to date a proper analytical method applicable for comparative screening of different antiparkinson products was not available. The objective of the present work was thus to develop and validate an analytical method for the simultaneous quantification of levodopa, carbidopa, benserazide and entacapone. The method should be applicable for quantifying samples from drug release experiments with marketed products and prototype formulations performed under compendial and biorelevant test conditions...
2017: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28810864/molecular-determination-of-antimicrobial-resistance-in-escherichia-coli-isolated-from-raw-meat-in-addis-ababa-and-bishoftu-ethiopia
#18
Yohannes Equar Messele, Reta Duguma Abdi, Shimels Tikuye Yalew, Desiye Tesfaye Tegegne, Bezina Arega Emeru, Gebremeskel Mamu Werid
BACKGROUND: Consumption of meat contaminated by E. coli causes a serious illness and even death to affected individuals. Recently the emerging of antibiotic resistant foodborne E. coli poses serious public health risks worldwide. However, little is known about the antibiotic resistance profile of E. coli in Ethiopia. This study aimed to determine the prevalence and Antimicrobial resistance (AMR) status of E. coli isolated from different type of meat. METHODS: Overall 292 samples were collected from December 2015 to April 2016 from slaughterhouses to determine the prevalence and AMR of E...
August 15, 2017: Annals of Clinical Microbiology and Antimicrobials
https://www.readbyqxmd.com/read/28809009/docking-and-virtual-screening-in-drug-discovery
#19
Maria Kontoyianni
Stages in a typical drug discovery organization include target selection, hit identification, lead optimization, preclinical and clinical studies. Hit identification and lead optimization are very much intertwined with computational modeling. Structure-based virtual screening (VS) has been a staple for more than a decade now in drug discovery with its underlying computational technique, docking, extensively studied. Depending on the objective, the parameters for VS may change, but the overall protocol is very straightforward...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28809005/resazurin-live-cell-assay-setup-and-fine-tuning-for-reliable-cytotoxicity-results
#20
José Á Rodríguez-Corrales, Jatinder S Josan
In vitro cytotoxicity tests allow for fast and inexpensive screening of drug efficacy prior to in vivo studies. The resazurin assay (commercialized as Alamar Blue(®)) has been extensively utilized for this purpose in 2D and 3D cell cultures, and high-throughput screening. However, improper or lack of assay validation can generate unreliable results and limit reproducibility. Herein, we report a detailed protocol for the optimization of the resazurin assay to determine relevant analytical (limits of detection, quantification, and linear range) and biological (growth kinetics) parameters, and, thus, provide accurate cytotoxicity results...
2017: Methods in Molecular Biology
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